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CAS No.: 220904-83-6

GW 5074 Catalog No. CSN18123

Synonyms: GW5074

GW5074 is an inhibitor of c-Raf1 kinase with IC50 of 9 nM.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 C-Raf

IC50:9nM
描述The mammalian Raf kinase family consists of A-Raf and B-Raf and c-Raf (or Raf 1). The c-Raf has been proven an upstream activator of mitogen-activated protein kinase (MAPK), which is an important group of mediators transducing signals from cell surface to nucleus under stimuli including cytokines, growth factors, exogenous pressure and mitogens. The RAF was also proven to be an oncogenic gene that was closely associated with tumorigenesis^[3]. GW5074 is a potent inhibitor of c-Raf with an IC₅₀ value of 9 nM. Treatment with GW5074 for 24 hours prevents LK-induced apoptosis in medium containing LK. Maximal protection against LK-induced apoptosis is observed at 1 μM. The activity of c-Raf immunoprecipitated from cultures treated with GW5074 in LK medium displayed a marked induction. Dispite its inhibition of c-Raf, treatment of neuronal cultures with GW5074 lea to an increase in the phosphorylation of ERK 1/2 suggesting that GW5074 treatment caused the activation of either A-Raf or B-Raf. Mice administered 3-NP display extensive bilateral striatal lesions. This degeneration is completely prevented by GW5074 when administered at a concentration of 5 mg/kg body weight^[4].
作用机制c-Raf is inhibited by phosphorylation at Ser259 with GW5074^[4].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03406364	Solid Tumor	Phase 1 Phase 2	Recruiting	December 31, 2019	Taiwan ... more >> Tri-Service General Hospital Recruiting Taipei, Nehu District, Taiwan, 114 Contact: Candace Liu +886-2-8792-3100 ext 19391 candaceliu@metagone.com.tw Collapse <<

参考文献

[1] Lei Y, Cao YX, et al. The Raf-1 inhibitor GW5074 and dexamethasone suppress sidestream smoke-induced airway hyperresponsiveness in mice. Respir Res. 2008 Nov 3;9:71.
[2] Yue X, Varga EV, et al. Chronic morphine-mediated adenylyl cyclase superactivation is attenuated by the Raf-1 inhibitor, GW5074. Eur J Pharmacol. 2006 Jul 1;540(1-3):57-9.
[3] Wei X, Zhao T, Ai K, Zhang Y, Li H, Yang J. c-Raf participates in adaptive immune response of Nile tilapia via regulating lymphocyte activation. Fish Shellfish Immunol. 2019;86:507-515.
[4] Chin PC, Liu L, Morrison BE, et al. The c-Raf inhibitor GW5074 provides neuroprotection in vitro and in an animal model of neurodegeneration through a MEK-ERK and Akt-independent mechanism. J Neurochem. 2004;90(3):595-608.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9196 mL
- 9.5980 mL
- 19.1960 mL
- 5 mM
- 0.3839 mL
- 1.9196 mL
- 3.8392 mL
- 10 mM
- 0.1920 mL
- 0.9598 mL
- 1.9196 mL

技术信息

CAS号

220904-83-6

储存条件

粉末: Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H8Br2INO2

运输

蓝冰

分子量

520.94

别名

GW5074

溶解度

DMSO	320.0 mg/mL (614.3 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	1.6 mg/mL	clear
PO	0.5% CMC-Na	51 mg/mL	suspension

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GW 5074 Catalog No. CSN18123

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